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Related Experiment Video

Updated: May 17, 2026

Microwave-assisted One-pot Synthesis of N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB)

Microwave-assisted One-pot Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate ([¹⁸F]SFB)

Published on: June 28, 2011

Accelerating SuFEx Reactions via Aryl Fluorosulfate Structural Engineering for Enhanced Covalent Targeted Cancer

Wenhui Gao¹, Chuangchuang Zhang¹, Daixi Li²

¹State Key Laboratory of Synergistic Chem-Bio Synthesis, Frontiers Science Center For Transformative Molecules, School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, People's Republic of China.

Angewandte Chemie (International Ed. in English)

|May 15, 2026

Summary

Researchers enhanced covalent protein drug development by optimizing aryl fluorosulfate (SuFEx) warheads. A meta-fluoro substituted warhead showed increased reactivity, improving drug delivery and anti-tumor efficacy.

Keywords:

accelerated SuFEx reaction aryl fluorosulfate warheads cancer therapy covalent targeting structural engineering

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Improving High Viscosity Extrusion of Microcrystals for Time-resolved Serial Femtosecond Crystallography at X-ray Lasers

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Published on: February 28, 2019

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Last Updated: May 17, 2026

Microwave-assisted One-pot Synthesis of N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB)

Microwave-assisted One-pot Synthesis of N-succinimidyl-4-[¹⁸F]fluorobenzoate ([¹⁸F]SFB)

Published on: June 28, 2011

Improving High Viscosity Extrusion of Microcrystals for Time-resolved Serial Femtosecond Crystallography at X-ray Lasers

Improving High Viscosity Extrusion of Microcrystals for Time-resolved Serial Femtosecond Crystallography at X-ray Lasers

Published on: February 28, 2019

Area of Science:

Medicinal Chemistry
Chemical Biology
Drug Discovery

Background:

Aryl fluorosulfate (SuFEx) warheads show promise for covalent protein drugs.
SuFEx reactivity is limited in complex protein environments.

Purpose of the Study:

To enhance SuFEx reactivity by modifying electronic and steric properties of warheads.
To develop novel covalent protein drugs with improved efficacy.

Main Methods:

Synthesis of maleimide-functionalized aryl fluorosulfate (MFS) with various substituents.
Conjugation of MFS warheads to Adnectin (EGFR-targeting protein).
Systematic investigation of SuFEx reactivity and covalent cross-linking efficiency.

Main Results:

The meta-fluoro (m-F) substituted MFS warhead exhibited the highest reactivity (3.5-fold increase).
m-F MFS-modified Adnectin enhanced intracellular accumulation (6.4-fold), tumor retention (3.0-fold), and anti-tumor efficiency (4.0-fold).

Conclusions:

Fine-tuning electronic and steric properties of warheads significantly enhances SuFEx reactivity.
Rational design of SuFEx-based warheads is crucial for developing effective covalent protein drugs.